Sarolan

Sarolaner is an isoxazoline used for the treatment of flea, tick or mite infestation in dogs due to its antiparasitic mode of action. The veterinary drug is marketed under the trade name Simparica® and has been approved in the EU since 2015 and in Switzerland since 2017 in the form of chewable tablets.
Der Wirkstoff verhindert eine Umweltkontamination mit Flöhen, da es die Flöhe vor der Eierlegung abtötet.

Pharmacodynamics

The mechanism of action of Sarolaner is based on blockade of GABA- and glutamate-gated chloride channels. Disruption of GABA and glutamate receptors inhibits the uptake of chloride ions into the central nervous system of mites and insects, resulting in increased nerve stimulation. This ultimately causes the death of the parasites.
Innerhalb von 28 Tagen nach der Gabe des Medikaments tritt die Wirkung bei Flöhen innerhalb von 8 Stunden nach der Anheftung ein, bei Zecken innerhalb von 12 Stunden nach der Anheftung. Zecken, die sich schon vor der Verabreichung auf dem Tier befanden, werden innerhalb von 24 Stunden abgetötet.

Pharmacokinetics

Sarolaner has a high bioavailability of 85%. The drug circulates almost completely bound to plasma proteins. The half-life is approximately 11 to 12 hours. It is excreted in the feces.

Drug Interactions

There are no known interactions with other active ingredients.

Toxicological data

Transient neurological signs, such as mild tremor and convulsions, were observed in some pups at 3 to 5 times the maximum treatment dose of 4 mg/kg, but the animals recovered without treatment.